Baumann Christa K, Castiglione-Gertsch Monica
Clinic and Policlinic for Medical Oncology, Inselspital, Bern, Switzerland.
Drugs. 2007;67(16):2335-53. doi: 10.2165/00003495-200767160-00004.
Endocrine treatments have been used in breast cancer since 1896, when Beatson reported on the results of oophorectomy for advanced breast cancer. In the second half of the last century, different endocrine-based compounds were developed and, in this review, the role of the selective estrogen receptor modulators (SERMs) and selective estrogen receptor down regulators (SERDs) in the postmenopausal setting are discussed. Tamoxifen is the most investigated and most widely used representative of these agents, and has been introduced in the advanced disease, in the neoadjuvant and adjuvant setting, and for the prevention of the disease. Its role has been challenged in recent years by the introduction of third-generation aromatase inhibitors that have proven higher activities than tamoxifen with different toxicity patterns. Several other SERMs have been investigated, but none have been clearly superior to tamoxifen. SERDs act as pure estrogen antagonists and should compare favourably to tamoxifen. For the time being, they have been used in the treatment of advanced breast cancers and their role in other settings still needs investigation. The increased use of aromatase inhibitors as first-line endocrine therapy has resulted in new discussions regarding the role that tamoxifen and other SERMs or SERDs may play in breast cancer. The sequencing of endocrine therapies in hormone-sensitive breast cancer remains a very important research issue.
自1896年Beatson报道晚期乳腺癌卵巢切除术的结果以来，内分泌治疗一直应用于乳腺癌。在上个世纪后半叶，研发出了不同的内分泌类化合物，在本综述中，将讨论选择性雌激素受体调节剂（SERM）和选择性雌激素受体下调剂（SERD）在绝经后情况下的作用。他莫昔芬是这些药物中研究最多、使用最广泛的代表药物，已被用于晚期疾病、新辅助和辅助治疗以及疾病预防。近年来，随着第三代芳香化酶抑制剂的引入，其作用受到了挑战，这些抑制剂已被证明比他莫昔芬具有更高的活性和不同的毒性模式。已经对其他几种SERM进行了研究，但没有一种明显优于他莫昔芬。SERD作为纯雌激素拮抗剂，应该比他莫昔芬更具优势。目前，它们已被用于治疗晚期乳腺癌，其在其他情况下的作用仍需研究。芳香化酶抑制剂作为一线内分泌治疗的使用增加，引发了关于他莫昔芬和其他SERM或SERD在乳腺癌中可能发挥的作用的新讨论。激素敏感性乳腺癌内分泌治疗的顺序仍然是一个非常重要的研究问题。
